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Asenapine hydrochloride

CAS No. : 1412458-61-7

MCE 站：Asenapine hydrochloride

产品活性：Asenapine hydrochloride，一种抗精神病药物，同时是 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) 和 Dopamine (D₂，D₃，D₄) 受体的拮抗剂，对 5-HT 受体的 K_i 值分别为 0.03-4.0 nM，多巴胺受体的 K_i 值分别为 1.3，0.42，1.1 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor  |  Dopamine Receptor

In Vitro: Relative to its D2 receptor affinity, Asenapine has a higher affinity for 5-HT_2C, 5-HT_2A, 5-HT_2B, 5-HT₇, 5-HT₆, α_2B and D3 receptors, suggesting stronger engagement of these targets at therapeutic doses. Asenapine behaves as a potent antagonist (pK_B) at 5-HT_1A (7.4), 5-HT1B (8.1), 5-HT_2A (9.0), 5-HT_2B (9.3), 5-HT_2C (9.0), 5-HT₆ (8.0), 5-HT₇ (8.5), D2 (9.1), D3 (9.1), α_2A (7.3), α_2B (8.3), α_2C (6.8) and H1 (8.4) receptors.

In Vivo: Asenapine is an atypical antipsychotic that is currently available for the treatment of schizophrenia and bipolar I disorder. Asenapine may have superior therapeutic effect on anxiety symptoms than other agents in rats. Asenapine has anxiolytic-like effects in the EPM and the defensive marble burying tests in mice.

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